This study involved developing a matrix-type transdermal therapeutic system comprising of ondansetron hydrochloride with 7:3 ratio of hydrophilic and hydrophobic polymeric combinations using solvent evaporation technique. The effects of permeation enhancers were studied at the concentrations of 2.5% and 5% using essential oils such as menthol oil, eucalyptus oil, clove oil, lemon grass oil and the blend of best volatile oil with Tween 20 dibutyl phthalate and glycerin were used as plasticizers. Formulated patches were evaluated for thickness, folding endurance, drug content, percent moisture absorption, percent moisture loss, tensile strength and water vapour transmission rate. There was no physicalchemical incompatibility between the drug and the polymers. The results of in vitro drug release studies showed that the blend of menthol oil and Tween 20 exhibited maximum release. The optimized formulation was found to be stable during the stability studies. The developed transdermal patches increase the efficacy and improve the bioavailability.
Objective: The objective of the present study was to formulate flurbiprofen (FLB) emulgel, evaluation of the formulations and the selection of an optimized formulation through in vitro drug release and drug content studies. Flurbiprofen is a non-steroidal anti-inflammatory drug (NSAID) requiring frequent administration and its chronic intake can lead to systemic side effects like gastric irritation and GI bleeding. The development of a dermal drug delivery system can overcome these side effects. Methods: The emulgel formulations were produced using different combinations of oil and emulsifying agents. Carbopol 940 was used as a gelling agent. The prepared emulgels were evaluated for general appearance, pH, spreadability, extrudability, drug content, in vitro drug release, average globule size and viscosity. Results: Optimized formulation F7 showed a better in vitro drug release compared to the marketed gel preparation. The stability study for the optimized formulation was carried out at 25 °C/60 % RH for 3 mo and the emulgel was found to be stable concerning the physical appearance, pH and drug content. Conclusion: The study revolved around the formulation of emulgel containing Flurbiprofen for dermal delivery of the drug. Emulgel was formulated with the purpose to enhance the permeation of poorly water-soluble drug FLB. The study concluded that the optimized emulgel containing FLB exhibited better in vitro drug release profile compared to the marketed formulation.
Objective:The main objective of this study was to formulate transdermal gels containing Flurbiprofen microsponges for controlled drug delivery. Methods: Microsponges containing Flurbiprofen and ethylcellulose were prepared by the quasi-emulsion solvent diffusion method. By varying the amount of drug and the polymer, seven batches of microsponges were formulated. Microsponges formed were characterized for surface morphology, thermal behavior, drug content, particle size, X-ray powder diffraction studies and in vitro drug dissolution studies. Results: SEM confirmed the spherical and the porous nature of the microsponges. Formulation F7 showed highest drug content and in vitro drug release of 92.74% at the end of 8 h and all the formulations followed zero order kinetics. Based on the results of drug content and in vitro release studies, formulation F4 was selected as the optimized batch and was incorporated into a carbopol gel base. The in vitro drug release from the microsponge gel was found to be extended over a longer period of time as compared to that from the marketed Flurbiprofen gel. Conclusion: Formulating Flurbiprofen in microsponges facilitated the controlled release of drug for long period of time thus eliminating the need of frequent dosing.
The buccal region of oral cavity is a interesting target for the drug of choice administration. To increase prevent first pass metabolism and bioavailability, Alfuzocin Hydrochloride is embedded in buccal film for a sustained release over a period of 8 hours. The purpose of this study was to develop formulations and systematically evaluate in vitro performances of buccoadhesive films of Alfuzocin hydrochloride using the polymers HPMC K100M, Sodium Alginate and Chitosan. The films were provided with a backing layer of Eudragit RS100 so as to get an unidirectional release pattern. The films were evaluated for their physical characteristics like weight, thickness, content uniformity, folding endurance, bioadhesive strength, surface pH, in vitro drug release, ex vivo buccal permeation and XRD studies. The films, which were prepared by the solvent casting method, were smooth and elegant in appearance; uniform in thickness, weight, and drug content; and showed good folding endurance. The mechanical properties reveal that the formulations were found to be strong but not brittle. The in vitro release data were fit to different equations and kinetic models viz. zero order, first order, higuchi’s plot and peppas plot. The best mucoadhesive performance and matrix controlled release was exhibited by the formulation A7 (2% HPMC K100 M and 2% Chitosan). The correlation coefficient value (r) indicates, the kinetic of drug release was zero order. Stability study of optimized films was done and it was found that both drug and buccal films were stable. It can be concluded that the present buccal formulation can be an ideal system to improve the bioavailability of the drug by avoiding hepatic first-pass metabolism.
The present study involved formulation of an in situ gelling system of brimonidine tartrate and timolol maleate for the treatment of glaucoma. Carbopol® 980 NF, xanthum gum and hydroxypropyl methylcellulose K4 M were used as polymers. The prepared in situ gelling systems were evaluated for clarity, appearance, texture analysis, pH, viscosity, rheological properties, in vitro gelation, isotonicity, drug content uniformity, in vitro release studies, microbiological evaluation, ex vivo release studies and stability testing. The results of the attenuated total reflectance spectroscopy and differential scanning calorimetry studies confirmed that there is no incompatibility between the drugs and the excipients. The formulations exhibited pseudoplastic rheology and formulation 3 showed the highest release of both the drugs from the formulation. The stability studies showed that the formulation was stable over the given period of time. Thus, it is evident that the in situ gelling system is a promising drug delivery system for the treatment of glaucoma.
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